32672-69-8

32672-69-8 structure

Name: Mesoridazine besylate
Chemical Name: mesoridazine besylate
CAS Number: 32672-69-8
Molecular Formula: C₂₇H₃₂N₂O₄S₃
Molecular Weight: 544.74900
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
Create Date: 2018-12-30 15:47:57
Modify Date: 2024-01-04 14:05:33
Mesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine benzenesulfonate is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells[1].Mesoridazine benzenesulfonate can be used for the research of schizophrenia, as well as certain other psychiatric disorders[1][2].

Name	mesoridazine besylate
Synonyms	benzenesulfonic acid,10-[2-(1-methylpiperidin-2-yl)ethyl]-2-methylsulfinylphenothiazine 10-[2-(1-Methyl-2-piperidinyl)ethyl]-2-(methylsulfinyl)-10H-phenothiazine Mesoridazine benzenesulfonate

Description	Mesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine benzenesulfonate is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells[1].Mesoridazine benzenesulfonate can be used for the research of schizophrenia, as well as certain other psychiatric disorders[1][2].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel
In Vitro	Mesoridazine blocks human ether-a-go-go-related gene (HERG) currents in a concentration-dependent manner (IC50 = 550 nM at 0 mV), block increased significantly over the voltage range where HERG activates and saturates at voltages eliciting maximal HERG channel activation[1]. Mesoridazine (15 mM; 24 h) shows total absorption of 15.94 ± 4.04% and 39.24 ± 5.11% in nude mouse and pig skin, respectively[3].
In Vivo	Mesoridazine (15 mM; topical administration; once or daily for 7 consecutive days) displays potent activity and a long period of analgesia at blocking cutaneous pain[3]. Mesoridazine (15 mM) shows intradermal concentration of 0.34 0.74 nmol/mg after topical application on nude mouse back for 6 h[3]. Animal Model: Eight-week-old female nude mice[3] Dosage: 15 mM Administration: Topical administration, once (analgesia test) or daily for 7 consecutive days (irritation test) Result: Showed analgesic effect. A slight transepidermal water loss (TEWL) increased from 7.8 to 9.9 g/m2/h was observed.
References	[1]. Zhi Su, et al. Mesoridazine: an open-channel blocker of human ether-a-go-go-related gene K+ channel. J Mol Cell Cardiol. 2004 Jan;36(1):151-60. [2]. I S M Salih, et al. Comparison of the effects of thioridazine and mesoridazine on the QT interval in healthy adults after single oral doses. Clin Pharmacol Ther. 2007 Nov;82(5):548-54. [3]. Liu KS, et al. Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment. Eur J Pharm Biopharm. 2016 Aug;105:59-68.

Boiling Point	570.5ºC at 760mmHg
Molecular Formula	C₂₇H₃₂N₂O₄S₃
Molecular Weight	544.74900
Flash Point	298.9ºC
Exact Mass	544.15200
PSA	130.81000
LogP	7.78380

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DB7176700

CAS REGISTRY NUMBER :: 32672-69-8

LAST UPDATED :: 199504

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C21-H26-N2-O-S2.C6-H6-O3-S

MOLECULAR WEIGHT :: 544.79

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 40 mg/kg

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction) Cardiac - other changes Nutritional and Gross Metabolic - changes in calcium

REFERENCE :: AEMED3 Annals of Emergency Medicine. (American College of Emergency Physicians, 1125 Executive Circle, Irving, TX 75038) Volume(issue)/page/year: 17,1074,1988 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6153 No. of Facilities: 92 (estimated) No. of Industries: 2 No. of Occupations: 3 No. of Employees: 4525 (estimated) No. of Female Employees: 4107 (estimated)

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
Precautionary Statements	P301 + P312 + P330
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xn: Harmful;
Risk Phrases	22
RIDADR	NONH for all modes of transport
RTECS	DB7176700

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